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交联剂对用于靶向给药的载药及释药壳聚糖水凝胶载体的影响。

Effect of Crosslinking Agents on Chitosan Hydrogel Carriers for Drug Loading and Release for Targeted Drug Delivery.

作者信息

Uddin Md Salah, Khand Suyash, Dong Chao

机构信息

Department of Mechanical Engineering, University of Texas Permian Basin, Odessa, TX 79762, USA.

Department of Chemistry, University of Texas Permian Basin, Odessa, TX 79762, USA.

出版信息

Gels. 2024 Jun 26;10(7):421. doi: 10.3390/gels10070421.

DOI:10.3390/gels10070421
PMID:39057444
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11276364/
Abstract

Numerous studies report on chitosan hydrogels in different forms, such as films, porous structures, nanoparticles, and microspheres, for biomedical applications; however, this study concentrates on their modifications with different crosslinking agents and observes their effects on drug loading and releasing capacities. Linear chitosan, along with chitosans crosslinked with two major crosslinkers, i.e., genipin and disulfide, are used to formulate three different hydrogel systems. The crosslinking process is heavily impacted by temperature and pH conditions. Three different drugs, i.e., thymoquinone, gefitinib, and erlotinib, are loaded to the hydrogels in de-ionized water solutions and released in phosphate-buffered solutions; thus, a total of nine combinations are studied and analyzed for their drug loading and releasing capabilities with ultraviolet-visible (UV-Vis) spectroscopy. This study finds that thymoquinone shows the lowest loading efficacy compared to the two other drugs in all three systems. Gefitinib shows stable loading and releasing regardless of crosslinking system, and the genipin-crosslinked system shows stable loading and releasing with all three drug molecules. These experimental results agree well with the findings of our previously published results conducted with molecular dynamics simulations.

摘要

许多研究报告了壳聚糖水凝胶以不同形式(如薄膜、多孔结构、纳米颗粒和微球)用于生物医学应用;然而,本研究专注于用不同交联剂对其进行改性,并观察其对药物负载和释放能力的影响。线性壳聚糖以及与两种主要交联剂(即京尼平与二硫键)交联的壳聚糖,被用于制备三种不同的水凝胶体系。交联过程受到温度和pH条件的严重影响。三种不同的药物,即百里醌、吉非替尼和厄洛替尼,在去离子水溶液中负载到水凝胶中,并在磷酸盐缓冲溶液中释放;因此,总共研究和分析了九种组合的药物负载和释放能力,采用紫外可见(UV-Vis)光谱法。本研究发现,在所有三种体系中,百里醌的负载效率与其他两种药物相比最低。吉非替尼无论交联体系如何都表现出稳定的负载和释放,而京尼平交联体系对所有三种药物分子都表现出稳定的负载和释放。这些实验结果与我们之前发表的分子动力学模拟结果非常吻合。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a97a/11276364/1a28e561e35a/gels-10-00421-g011.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a97a/11276364/719721de869c/gels-10-00421-g009.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a97a/11276364/1a28e561e35a/gels-10-00421-g011.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a97a/11276364/b45dde306397/gels-10-00421-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a97a/11276364/98b1edf2babd/gels-10-00421-g003.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a97a/11276364/34e2c612b8d5/gels-10-00421-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a97a/11276364/719721de869c/gels-10-00421-g009.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a97a/11276364/1a28e561e35a/gels-10-00421-g011.jpg

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